3067695-20-6
Chemical Structure
PROTAC FLT3/JAK2/BRD4 Degrader-1
- CAS No.: 3067695-20-6
- Formula:C44H51FN10O7S
- Molecular Weight:883.00
IUPAC Name: N-(3-((2-((4-(4-(6-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)hexanoyl)piperazin-1-yl)-3-fluorophenyl)amino)-5-methylpyrimidin-4-yl)amino)phenyl)-2-methylpropane-2-sulfonamide
InChIKey: DPKSODWBQFFQAR-UHFFFAOYSA-N
SMILES: CC1=C(N=C(N=C1)NC2=CC=C(C(F)=C2)N3CCN(CC3)C(CCCCCNC4=CC=C5C(C(N(C5=O)C6CCC(NC6=O)=O)=O)=C4)=O)NC7=CC=CC(NS(C(C)(C)C)(=O)=O)=C7
Biological Activity: PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML)[1].
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PROTAC FLT3/JAK2/BRD4 Degrader-1 | PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). | |||||||||||||||||||||
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Keywords
